Fibrosis is a pathologic process, characterized by overproduction of extracellular matrix (ECM) as a response to tissue injury. Nearly 45% of all deaths in the developed world can be attributed to some type of chronic fibroproliferative disease. Despite their high prevalence, current therapeutic options for fibrotic diseases are quite limited to elimination of triggering stimuli and organ transplantation. No effective agent exists that can directly halt the disease progression at the cellular level, which represents a major unmet medical need. Pharmacological modulation of the αvβ1 integrin by small molecules presents one route to test the role of the αvβ1 integrin in tissue fibrosis. Most integrins contain either an αv chain or β1 chain, and targeting either subunit by itself provides little specificity. Accordingly, there is a need in the art for potent, selective αvβ1 integrin inhibitors. Provided herein are solutions to these and other problems in the art.